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JR-AB2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM). JR-AB2-011 has anti-glioblastoma multiforme (GBM) properties[1]. mTORC2|0.36 μM (IC50)

JR-AB2-011 (1 μM; 24 hours) has good anti-GBM properties, blocks mTORC2 signaling and Rictor association with mTOR[1].JR-AB2-011 (0.5-2 μM; 48 hours) displays the least toxicity to normal neurons with no significant cytotoxic effects for concentrations up to 10 mM compared to CID613034[1]. Apoptosis Analysis[1] Cell Line: U87 GBM cells; LN229 GBM cells

Mice receiving JR-AB2-011 (4 mg/kg; daily i.p. for 10 days; 20 mg/kg; daily i.p. for 10 days) at either dosing regimen display marked inhibition of tumor growth rate (JR-AB2-011 at 4 mg/kg/d; 74% inhibition at end of dosing period; tumor growth delay 10.0 days; JR-AB2-011 at 20 mg/kg/d; 80% inhibition at end of dosing period; tumor growth delay 12.0 days) as compared to mice receiving vehicle alone[1]. Animal Model: LN229 cells in female C.B.-17-scid (Taconic) mice[1]

[1]. Benavides-Serrato A, et al. Specific blockade of Rictor-mTOR association inhibits mTORC2 activity and is cytotoxic in glioblastoma. PLoS One. 2017 Apr 28;12(4):e0176599.

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